CY1118524T1 - 2-(αζαϊνδολ-2-υλο)βενζιμιδαζολια ως pad4 αναστολεις - Google Patents
2-(αζαϊνδολ-2-υλο)βενζιμιδαζολια ως pad4 αναστολειςInfo
- Publication number
- CY1118524T1 CY1118524T1 CY20171100128T CY171100128T CY1118524T1 CY 1118524 T1 CY1118524 T1 CY 1118524T1 CY 20171100128 T CY20171100128 T CY 20171100128T CY 171100128 T CY171100128 T CY 171100128T CY 1118524 T1 CY1118524 T1 CY 1118524T1
- Authority
- CY
- Cyprus
- Prior art keywords
- hydrogen
- 6alkyl
- alkyl
- pad4
- azaindol
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Ενώσεις του τύπου (I) όπου: η R1 είναι υδρογόνο ή C1-6 αλκύλιο· η R2 είναι υδρογόνο, C1-6 αλκύλιο, υπεραλογονομεθυλοC0-5αλκυλο-O-, ή C1-6άλκοξυ· η R3 είναι υδρογόνο, C1-6αλκύλιο, ή C1-6αλκοξυC1-6αλκύλιο· η R4 είναι υδρογόνο, C1-6αλκύλιο, υπεραλογονομεθυλοC1-6αλκύλιο· ή μη υποκατεστημένο C3-6κυκλοαλκυλοC1-6αλκύλιο· η Α είναι C-R5 ή Ν· η Β είναι C-R6 ή Ν· η D είναι C-R7 ή Ν· με τον όρο ότι τουλάχιστον μία των Α, Β και D είναι Ν· η R5 είναι υδρογόνο ή C1-6αλκύλιο· η R6, είναι υδρογόνο ή C1-6αλκύλιο· η R7 είναι υδρογόνο, C1-6αλκύλιο, C1-6άλκοξυ, ή ύδροξυ· η R8 είναι υδρογόνο ή C1-6αλκύλιο, με τον όρο ότι μία των R4 και R8 είναι υδρογόνο· η R9 είναι υδρογόνο ή ύδροξυ· η R10 είναι υδρογόνο ή C1-6αλκύλιο· και τα άλατα αυτών είναι PAD4 αναστολείς και αναμένεται να είναι χρήσιμα στη θεραπευτική αγωγή διαφόρων διαταραχών, για παράδειγμα ρευματοειδούς αρθρίτιδας, αγγειίτιδας, συστημικού ερυθηματώδη λύκου, ελκωτικής κολίτιδας, καρκίνου, κυστικής ίνωσης, άσθματος, δερματικού ερυθηματώδους λύκου και ψωρίασης.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2012/064649 WO2014015905A1 (en) | 2012-07-26 | 2012-07-26 | 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1118524T1 true CY1118524T1 (el) | 2017-07-12 |
Family
ID=49996626
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20171100128T CY1118524T1 (el) | 2012-07-26 | 2017-01-27 | 2-(αζαϊνδολ-2-υλο)βενζιμιδαζολια ως pad4 αναστολεις |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US9127003B2 (el) |
| EP (1) | EP2877467B1 (el) |
| JP (1) | JP6063567B2 (el) |
| KR (1) | KR101916443B1 (el) |
| CN (1) | CN104470919B (el) |
| AU (1) | AU2012386257B2 (el) |
| BR (1) | BR112015001545B1 (el) |
| CA (1) | CA2879341C (el) |
| CY (1) | CY1118524T1 (el) |
| DK (1) | DK2877467T3 (el) |
| ES (1) | ES2609126T3 (el) |
| HR (1) | HRP20161530T1 (el) |
| HU (1) | HUE033294T2 (el) |
| IN (1) | IN2014KN02935A (el) |
| LT (1) | LT2877467T (el) |
| PL (1) | PL2877467T3 (el) |
| PT (1) | PT2877467T (el) |
| RS (1) | RS55684B1 (el) |
| RU (1) | RU2611010C2 (el) |
| SI (1) | SI2877467T1 (el) |
| SM (2) | SMT201700052T1 (el) |
| WO (1) | WO2014015905A1 (el) |
Families Citing this family (38)
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| BR112017024678A2 (pt) * | 2015-05-21 | 2018-07-31 | Glaxosmithkline Intellectual Property Development Limited | derivados de benzoimidazol como inibidores de pad4 |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| AR107032A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| JP6926126B2 (ja) * | 2016-02-23 | 2021-08-25 | パドロック・セラピューティクス・インコーポレイテッドＰａｄｌｏｃｋ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | Ｐａｄ４のヘテロアリール阻害剤 |
| CN107188867A (zh) * | 2016-03-14 | 2017-09-22 | 中国科学院天津工业生物技术研究所 | 精氨酸脱亚氨酶4的抑制剂 |
| CN109790162B (zh) * | 2016-07-27 | 2022-06-28 | 帕德罗科治疗公司 | Pad4的共价抑制剂 |
| EP3510025B1 (en) * | 2016-09-12 | 2022-06-29 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| WO2018102262A1 (en) * | 2016-12-02 | 2018-06-07 | University Of Massachusetts | Inhibitors of protein arginine deiminases (pads) and methods of preparation and use thereof |
| CN108689946B (zh) * | 2017-04-12 | 2022-10-18 | 中国科学院上海药物研究所 | 2-取代硫基乙酰胺类化合物及其制备方法和应用 |
| IL273428B2 (en) * | 2017-09-22 | 2023-09-01 | Jubilant Epipad LLC | Heterocyclic compounds as pad inhibitors |
| CN111225915B (zh) * | 2017-10-18 | 2023-03-07 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的咪唑并吡啶化合物 |
| BR112020008851A2 (pt) | 2017-11-06 | 2020-10-20 | Jubilant Prodel LLC | composto da fórmula i, processo de preparação de compostos da fórmula i, composição farmacêutica, método para o tratamento e/ou prevenção de várias doenças, uso, método para o tratamento de câncer, método de tratamento de câncer e método para o tratamento e/ou prevenção de câncer e doenças infecciosas |
| JP7368369B2 (ja) | 2017-11-24 | 2023-10-24 | ジュビラント・エピスクライブ・エルエルシー | Ｐｒｍｔ５阻害剤としてのヘテロ環式化合物 |
| WO2019161803A1 (zh) * | 2018-02-26 | 2019-08-29 | 南京药捷安康生物科技有限公司 | 肽酰精氨酸脱亚胺酶抑制剂及其用途 |
| JP7279063B6 (ja) | 2018-03-13 | 2024-02-15 | ジュビラント プローデル エルエルシー | Ｐｄ１／ｐｄ－ｌ１相互作用／活性化の阻害剤としての二環式化合物 |
| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| WO2020033490A1 (en) | 2018-08-08 | 2020-02-13 | Bristol-Myers Squibb Company | Substituted thienopyrroles as pad4 inhibitors |
| AU2019318415A1 (en) * | 2018-08-08 | 2021-03-25 | Bristol-Myers Squibb Company | Substituted benzimidazoles as PAD4 inhibitors |
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| CN109369513B (zh) * | 2018-11-20 | 2020-08-25 | 都创(上海)医药科技有限公司 | 一种fbdd常用分子片段的制备方法 |
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2012
- 2012-07-26 SI SI201230769A patent/SI2877467T1/sl unknown
- 2012-07-26 LT LTEP12740581.9T patent/LT2877467T/lt unknown
- 2012-07-26 BR BR112015001545-0A patent/BR112015001545B1/pt active IP Right Grant
- 2012-07-26 DK DK12740581.9T patent/DK2877467T3/en active
- 2012-07-26 EP EP12740581.9A patent/EP2877467B1/en active Active
- 2012-07-26 RS RS20170121A patent/RS55684B1/sr unknown
- 2012-07-26 AU AU2012386257A patent/AU2012386257B2/en active Active
- 2012-07-26 CA CA2879341A patent/CA2879341C/en active Active
- 2012-07-26 ES ES12740581.9T patent/ES2609126T3/es active Active
- 2012-07-26 JP JP2015523426A patent/JP6063567B2/ja active Active
- 2012-07-26 US US14/416,937 patent/US9127003B2/en active Active
- 2012-07-26 KR KR1020157005099A patent/KR101916443B1/ko active Active
- 2012-07-26 PT PT127405819T patent/PT2877467T/pt unknown
- 2012-07-26 CN CN201280074868.5A patent/CN104470919B/zh active Active
- 2012-07-26 RU RU2014152456A patent/RU2611010C2/ru active
- 2012-07-26 HR HRP20161530TT patent/HRP20161530T1/hr unknown
- 2012-07-26 PL PL12740581T patent/PL2877467T3/pl unknown
- 2012-07-26 WO PCT/EP2012/064649 patent/WO2014015905A1/en not_active Ceased
- 2012-07-26 SM SM20170052T patent/SMT201700052T1/it unknown
- 2012-07-26 IN IN2935KON2014 patent/IN2014KN02935A/en unknown
- 2012-07-26 HU HUE12740581A patent/HUE033294T2/en unknown
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2015
- 2015-08-03 US US14/816,246 patent/US9518054B2/en active Active
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2016
- 2016-11-15 US US15/352,340 patent/US9833449B2/en active Active
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2017
- 2017-01-24 SM SM201700052T patent/SMT201700052B/it unknown
- 2017-01-27 CY CY20171100128T patent/CY1118524T1/el unknown
- 2017-11-20 US US15/817,562 patent/US10039755B2/en active Active
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